Effect of CYP3A perpetrators on ibrutinib exposure in healthy participants

Pharmacology Research and Perspectives

Volumn 3, Issue 4, 2015, Pages

  de Jong, Jan ^a   Skee, Donna ^b   Murphy, Joe ^b   Sukbuntherng, Juthamas ^c   Hellemans, Peter ^a   Smit, Johan ^a   de Vries, Ronald ^a   Jiao, Juhui James ^b   Snoeys, Jan ^a   Mannaert, Erik ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b JANSSEN RESEARCH AND DEVELOPMENT   (United States)

^c PHARMACYCLICS INC   (United States)

Author keywords

Bioavailability; CYP3A perpetrators; grapefruit juice; ibrutinib; ketoconazole; rifampin

Indexed keywords

CYTOCHROME P450 3A; CYTOCHROME P450 3A INHIBITOR; IBRUTINIB; KETOCONAZOLE; RIFAMPICIN;

ADULT; ARTICLE; B CELL LYMPHOMA; BODY MASS; DRUG DETERMINATION; DRUG EFFICACY; DRUG EXPOSURE; DRUG SAFETY; FEMALE; GRAPEFRUIT JUICE; HUMAN; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; METABOLITE; NORMAL HUMAN; PRIORITY JOURNAL;

EID: 84962928704     PISSN: None     EISSN: 20521707     Source Type: Journal    
DOI: 10.1002/prp2.156     Document Type: Article

References (25)

1. Advani RH, Buggy JJ, Sharman JP, Smith SM, Boyd TE, Grant B, et al. (2013). Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies. J Clin Oncol 31: 88–94.
2. Bailey DG, Arnold JM, Bend JR, Tran LT, Spence JD (1995). Grapefruit juice-felodipine interaction: reproducibility and characterization with the extended release drug formulation. Br J Clin Pharmacol 40: 135–140.
3. Bjorkhem-Bergman L, Backstrom T, Nylen H, Ronquist-Nii Y, Bredberg E, Andersson TB, et al. (2013). Comparison of endogenous 4beta-hydroxycholesterol with midazolam as markers for CYP3A4 induction by rifampicin. Drug Metab Dispos 41: 1488–1493.
4. Byrd JC, Furman RR, Coutre SE, Flinn IW, Burger JA, Blum KA, et al. (2013). Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia. N Engl J Med 369: 32–42.
5. Ducharme MP, Warbasse LH, Edwards DJ (1995). Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 57: 485–491.
6. Dutreix C, Lorenzo S, Wang Y (2014). Comparison of two endogenous biomarkers of CYP3A4 activity in a drug-drug interaction study between midostaurin and rifampicin. Eur J Clin Pharmacol 70: 915–920.
7. Fuentes-Panana EM, Bannish G, Monroe JG (2004). Basal B-cell receptor signaling in B lymphocytes: mechanisms of regulation and role in positive selection, differentiation, and peripheral survival. Immunol Rev 197: 26–40.
8. Garg SK, Kumar N, Bhargava VK, Prabhakar SK (1998). Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy. Clin Pharmacol Ther 64: 286–288.
9. Guo LQ, Yamazoe Y (2004). Inhibition of cytochrome P450 by furanocoumarins in grapefruit juice and herbal medicines. Acta Pharmacol Sin 25: 129–136.
10. Guo LQ, Taniguchi M, Xiao YQ, Baba K, Ohta T, Yamazoe Y (2000). Inhibitory effect of natural furanocoumarins on human microsomal cytochrome P450 3A activity. Jpn J Pharmacol 82: 122–129.
11. Hanley MJ, Cancalon P, Widmer WW, Greenblatt DJ (2011). The effect of grapefruit juice on drug disposition. Expert Opin Drug Metab Toxicol 7: 267–286.
12. Honigberg LA, Smith AM, Sirisawad M, Verner E, Loury D, Chang B, et al. (2010). The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA 107: 13075–13080.
13. ™. 2014. Summary of product information European Medicines Agency. Available at http://www.medicines.org.uk/emc/medicine/29383 (accessed January 9, 2015).
14. de Jong J, Sukbuntherng J, Skee D, Murphy J, O'Brien S, Byrd JC, et al. (2015). The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia. Cancer Chemother Pharmacol 75: 907–916.
15. Sukbuntherng J, de Jong J, Skee D, Pak Y, Fardis M, O'Brien S, et al. (2014) Pharmacokinetics and safety of ibrutinib with concomitant use of CYP3A inhibitors in patients with B-cell malignancies. Presented at the American College of Clinical Pharmacy (ACCP) annual meeting, Austin, Texas, Oct 12–15.
16. Kuppers R (2005). Mechanisms of B-cell lymphoma pathogenesis. Nat Rev Cancer 5: 251–262.
17. Marasanapalle VP, Boinpally RR, Zhu H, Grill A, Tang F (2011). Correlation between the systemic clearance of drugs and their food effects in humans. Drug Dev Ind Pharm 37: 1311–1317.
18. Marde Arrhen Y, Nylen H, Lovgren-Sandblom A, Kanebratt KP, Wide K, Diczfalusy U (2013). A comparison of 4beta-hydroxycholesterol: cholesterol and 6beta-hydroxycortisol: cortisol as markers of CYP3A4 induction. Br J Clin Pharmacol 75: 1536–1540.
19. Marostica E, Sukbuntherng J, Loury D, de Jong J, de Trixhe XW, Vermeulen A, et al. (2015). Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies. Cancer Chemother Pharmacol 75: 111–121.
20. Parmar S, Patel K, Pinilla-Ibarz J (2014). Ibrutinib (imbruvica): a novel targeted therapy for chronic lymphocytic leukemia. P T 39: 483–519.
21. de Vries R, Smit JW, Hellemans P, Jiao J, Murphy J, Skee D, et al. (2015) Stable Isotope-Intravenous Microdose for Absolute Bioavailability and Effect of Grapefruit Juice on Ibrutinib in Healthy Adults. Br J Clin Pharmacol: In press.
22. Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, et al. (2015). Absorption, metabolism, and excretion of oral 14C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos 43: 289–297.
23. Seidegard J, Nyberg L, Borga O (2012). Differentiating mucosal and hepatic metabolism of budesonide by local pretreatment with increasing doses of ketoconazole in the proximal jejunum. Eur J Pharm Sci 46: 530–536.
24. Shoaf SE, Mallikaarjun S, Bricmont P (2012). Effect of grapefruit juice on the pharmacokinetics of tolvaptan, a non-peptide arginine vasopressin antagonist, in healthy subjects. Eur J Clin Pharmacol 68: 207–211.
25. Veronese ML, Gillen LP, Burke JP, Dorval EP, Hauck WW, Pequignot E, et al. (2003). Exposure-dependent inhibition of intestinal and hepatic CYP3A4 in vivo by grapefruit juice. J Clin Pharmacol 43: 831–839.